The TRPM4 channel inhibitor 9-phenanthrol

Authors

  • R Guinamard,

    Corresponding author
    1. EA 4650, Groupe Signalisation, Electrophysiologie et Imagerie des Lésions d'Ischémie-Reperfusion Myocardique, UCBN, Normandie Université, Caen, France
    2. Department of Applied Science, The College of William and Mary, Williamsburg, VA, USA
    • Correspondence

      Romain Guinamard, Groupe Signalisation, Electrophysiologie et Imagerie des Lésions d'Ischémie/Reperfusion Myocardique, EA4650, Université de Caen Basse Normandie, Sciences D, Esplande de la Paix, CS 14032, 14032 Caen Cedex 5, France. E-mail: romain.guinamard@unicaen.fr

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  • T Hof,

    1. EA 4650, Groupe Signalisation, Electrophysiologie et Imagerie des Lésions d'Ischémie-Reperfusion Myocardique, UCBN, Normandie Université, Caen, France
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  • C A Del Negro

    1. Department of Applied Science, The College of William and Mary, Williamsburg, VA, USA
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Abstract

The phenanthrene-derivative 9-phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin (TRPM) 4 channel, a Ca2+-activated non-selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity of the drug for TRPM4. In addition, 9-phenanthrol modulates a variety of physiological processes through TRPM4 current inhibition and thus exerts beneficial effects in several pathological conditions. 9-Phenanthrol modulates smooth muscle contraction in bladder and cerebral arteries, affects spontaneous activity in neurons and in the heart, and reduces lipopolysaccharide-induced cell death. Among promising potential applications, 9-phenanthrol exerts cardioprotective effects against ischaemia-reperfusion injuries and reduces ischaemic stroke injuries. In addition to reviewing the biophysical effects of 9-phenanthrol, here we present information about its appropriate use in physiological studies and possible clinical applications.

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